Structure-Activity Relationships of Baicalein and its Analogs as Novel TSLP Inhibitors

Scientific Reports
Bernie Byunghoon ParkYoung Ho Jeon

Abstract

Thymic stromal lymphopoietin (TSLP) plays an important role in the differentiation and proliferation of Th2 cells, resulting in eosinophilic inflammation and numerous allergic diseases. Baicalein (1), a major component of Scutellaria baicalensis, was found to be the first small molecule to block TSLP signaling pathways. It inhibited effectively eosinophil infiltration in house dust mite-induced and ovalbumin-challenged mouse models. Structure-activity relationship studies identified compound 11a, a biphenyl flavanone analog, as a novel human TSLP inhibitor for the discovery and development of new anti-allergic drugs.

References

Dec 1, 1975·Japanese Journal of Pharmacology·H NagaiA Koda
Aug 1, 1979·Proceedings of the National Academy of Sciences of the United States of America·J MillerM A Raftery
Jun 4, 1999·Journal of Medicinal Chemistry·L CostantinoA Albasini
Mar 20, 2001·American Journal of Respiratory and Critical Care Medicine·A TomkinsonE W Gelfand
Jul 28, 2001·Cytogenetics and Cell Genetics·Y TonozukaT Kitamura
Jan 7, 2004·International Archives of Allergy and Immunology·Sampson B SarpongSteven R Kleeberger
Mar 15, 2005·Current Opinion in Allergy and Clinical Immunology·P Ly NgocJuan C Celedón
Aug 8, 2006·The Journal of Allergy and Clinical Immunology·Hamida Hammad, Bart N Lambrecht
Apr 20, 2007·Phytochemistry·Angelyne BenavidesCosimo Pizza
Dec 19, 2008·Disease Models & Mechanisms·Anthony T Nials, Sorif Uddin
Oct 27, 2010·Proceedings of the National Academy of Sciences of the United States of America·Yrina RochmanWarren J Leonard
May 3, 2011·Organic Letters·Hiroyuki NemotoShuji Akai
Dec 16, 2011·Bioorganic & Medicinal Chemistry Letters·Thaís Moreira OsórioArtur Smânia
Jan 26, 2012·Journal of Natural Products·Chien-Chang ShenChien-Chih Chen
Mar 27, 2012·Bioorganic & Medicinal Chemistry Letters·Dayong ShiTao Wang
May 24, 2012·Journal of Visualized Experiments : JoVE·Aravind T ReddyRaju C Reddy
Oct 26, 2012·The Journal of Organic Chemistry·Chun WuPatrick S Mariano
May 7, 2013·Current Opinion in Pharmacology·Martijn J SchuijsBart N Lambrecht
May 7, 2013·PloS One·Ulaganathan MabalirajanSurendra Kumar Sharma
May 21, 2013·Nature Immunology·Paula Licona-LimónRichard A Flavell
Jul 6, 2013·Nature Reviews. Immunology·William C GauseJudith E Allen
Feb 28, 2014·Chemical & Pharmaceutical Bulletin·Shu-Ting ChungAn-Rong Lee
May 23, 2014·The New England Journal of Medicine·Gail M GauvreauJane R Parnes
Dec 5, 2014·Journal of Leukocyte Biology·Taylor A Doherty
Oct 2, 2015·Journal of the American Society for Mass Spectrometry·Jingjing ZhangJohn S Klassen
Oct 17, 2015·Nature Reviews. Drug Discovery·Namita A GandhiGeorge D Yancopoulos
Dec 22, 2015·The International Journal of Tuberculosis and Lung Disease : the Official Journal of the International Union Against Tuberculosis and Lung Disease·S Ehteshami-AfsharM Sadatsafavi
Sep 13, 2016·Journal of Natural Products·Mohamed A ZakiIlias Muhammad
Oct 18, 2016·The Journal of Allergy and Clinical Immunology·Fahima MadouriDieudonnée Togbe
Dec 22, 2016·Journal of Structural Biology·Ji Young ParkKa Young Chung
Jun 2, 2017·Organic & Biomolecular Chemistry·Midori A AraiMasami Ishibashi
Sep 21, 2017·Bioorganic & Medicinal Chemistry Letters·Seonghu ParkYoungjoo Byun
Dec 10, 2017·Scientific Reports·Dries Van RompaeyHans De Winter

Citations

Feb 21, 2020·Drugs·Maria Gabriella MateraMario Cazzola
Aug 28, 2020·Frontiers in Immunology·Iva Marković, Savvas N Savvides

Methods Mentioned

BETA
enzyme-linked immunosorbent assay
ELISA
NMR
chemical exchange
pull-down
microscale thermophoresis
bronchoalveolar lavage
flow cytometry
column chromatography
gel-filtration

Related Concepts

Analogs & derivatives
Cell Differentiation Process
Hypersensitivity
Ovalbumin
Baicalein
T-helper Cell Type 2
Inhibitors
Cell Proliferation
S-11-A
TSLP protein, human

Related Feeds

Allergy and Asthma

Allergy and asthma are inflammatory disorders that are triggered by the activation of an allergen-specific regulatory t cell. These t cells become activated when allergens are recognized by allergen-presenting cells. Here is the latest research on allergy and asthma.

Related Papers

Seikagaku. The Journal of Japanese Biochemical Society
Kazuhiko Arima
Lin chuang er bi yan hou tou jing wai ke za zhi = Journal of clinical otorhinolaryngology, head, and neck surgery
Meili Xu, Yongqing Guo
Lin chuang er bi yan hou tou jing wai ke za zhi = Journal of clinical otorhinolaryngology, head, and neck surgery
Yu ZhongXuping Xiao
© 2021 Meta ULC. All rights reserved